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Effects of Oral Administration of Androstenedione on Plasma Androgens in Young Women Using Hormonal Contraception

Departments of Forensic Science and Drug Monitoring (Drug Control Centre) (T.B., D.A.C., S.D., A.T.K.), Pharmacy (A.J.H.), and Nutrition (A.R.L.), King’s College London, London SE1 9NH, United Kingdom; and Department of Chemical Pathology (M.J.W.), St. Thomas’ Hospital, London SE1 7EH, United Kingdom

Address all correspondence and requests for reprints to: Andrew T. Kicman, Department of Forensic Science and Drug Monitoring (Drug Control Centre), King’s College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NH, United Kingdom. E-mail: andrew.kicman{at}kcl.ac.uk.

Androstenedione as a dietary supplement has been targeted at the sporting community, but there are limited data regarding its effects on plasma androgens in young women. A double-blind, cross-over study was undertaken involving 10 women (20–32 yr) using hormonal contraception. Because contamination of supplements has been reported, an in-house oral formulation was prepared containing purified androstenedione, the control being lactose only. After oral administration of a single dose of androstenedione (100 mg), blood was collected frequently up to 8 h and at 24 h. Maximum plasma androgen concentrations observed between volunteers were well above the upper limit of reference ranges for women, being 121–346 nmol/liter for androstenedione, 14–54 nmol/liter for testosterone (T), 11–32 nmol/liter for 5-dihydrotestosterone, and 23–90 nmol/liter for 3-androstanediol glucuronide. The free androgen index and T concentration changed in a similar manner. The mean change in area under the plasma concentration-time curve (0–24 h), compared with control data were: androstenedione approximately 7-fold, T approximately 16-fold, 5-dihydrotestosterone approximately 9-fold, and 3-androstanediol glucuronide approximately 5-fold; the mean conversion ratio of androstenedione to T was 12.5% (range 7.8–21.6%). Increases in T area under the plasma concentration-time curve were correlated with SHBG concentration (r = 0.80; P = 0.005). Formulation characteristics and SHBG levels appear to be important factors when considering plasma androgen increases after acute androstenedione administration.